Published date: 2024-07-17 15:06:38
CAS number: 870653-45-5
Name: PAP-1
Price:
$320.0/50mg
$500.0/100mg
$900.0/250mg
Purity: 98.0%
Stocking period: 3 Day
Stock: 3
Product Webpage: https://www.dcchemicals.com/product_show-DC23946.html
Detail Product Information:
PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2].
Name: DC Chemicals Limited Recommended
Chemsrc Level: Verified
Product #: 34952
Tel: 58447131
Address: Jinyu Rd100, pudong
Area: China(Mainland)
Contact: Tony Cao
Contact Phone #: 13564518121
Email: sales@dcchemicals.com
Website: http://www.dcchemicals.com
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Name: Shanghai Nianxing Industrial Co., Ltd
Area: China
Price:
$320.0/50mg
$500.0/100mg
$900.0/250mg
Contact: Yang
Product Detail: PAP-1
Name: Shanghai Jizhi Biochemical Technology Co., Ltd
Area: China
Price:
$320.0/50mg
$500.0/100mg
$900.0/250mg
Contact: Liu jia
Product Detail: PAP-1
Name: DC Chemicals Limited
Area: China
Price:
$320.0/50mg
$500.0/100mg
$900.0/250mg
Contact: Tony Cao
Product Detail: PAP-1
Name: ShangHai DC Chemicals Co.,Ltd
Area: China
Price:
$320.0/50mg
$500.0/100mg
$900.0/250mg
Contact: Tony Lai
Product Detail: PAP-1
Name: Dayang Chem (Hangzhou) Co., Ltd.
Area: China
Price:
$320.0/50mg
$500.0/100mg
$900.0/250mg
Contact: Ms Wang
Product Detail: 4-(4-PHENOXYBUTOXY)-7H-FURO[3,2-G]CHROMEN-7-ONE
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2024-07-15 PAP-1
2019-03-05 PAP-1
2022-11-29 PAP-1
2021-07-26 4-(4-PHENOXYBUTOXY)-7H-FURO[3,2-G]CHROMEN-7-ONE
2022-05-12 PAP-1,5-(4-Phenoxybutoxy)psoralen
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